A report on Methylphenidate

Addiction experts in psychiatry, chemistry, pharmacology, forensic science, epidemiology, and the police and legal services engaged in delphic analysis regarding 20 popular recreational drugs. Methylphenidate was ranked 13th in dependence, 12th in physical harm, and 18th in social harm.
Packaging of a formulation of methylphenidate advises against crushing the tablets. It is placed under Schedule X of the Indian drug scheduling system. Schedule X medications typically hold abusable medications such as barbiturates or stimulants such as amphetamines.
German "Ritalin" brand methylphenidate.
Indian "AddWize" branded instant release and extended release formulations costing US$1.9 for strip of instant release and US$2.9 for a strip of AddWize extended release.
Clockwise from top: Concerta 18 mg, Medikinet 5 mg, Methylphenidat TAD 10 mg, Ritalin 10 mg, Medikinet XL 30 mg.
Structural formula for the substance among Ritalin tablet series. (Ritalin, Ritalin LA, Ritalin SR.) The volume of distribution was 2.65±1.11 L/kg for d-methylphenidate and 1.80±0.91 L/kg for l-methylphenidate subsequent to swallow of Ritalin tablet.
Structural formula for the substance inside Concerta tablet. Following administration of Concerta, plasma concentrations of the l-isomer were approximately 1/40 the plasma concentrations of the d-isomer.
Ritalin 10 mg tablet
Legal warning printed on Ritalin packaging

Central nervous system stimulant medication used to treat attention deficit hyperactivity disorder (ADHD) and, to a lesser extent, narcolepsy.

- Methylphenidate

52 related topics with Alpha

Overall

Amphetamine

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Strong central nervous system (CNS) stimulant that is used in the treatment of attention deficit hyperactivity disorder (ADHD), narcolepsy, and obesity.

Strong central nervous system (CNS) stimulant that is used in the treatment of attention deficit hyperactivity disorder (ADHD), narcolepsy, and obesity.

Psychostimulants like methylphenidate and amphetamine are effective in treating ADHD because they increase neurotransmitter activity in these systems.

Ritalin: 20 mg sustained-release (SR) tablets

Stimulant

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Overarching term that covers many drugs including those that increase activity of the central nervous system and the body, drugs that are pleasurable and invigorating, or drugs that have sympathomimetic effects.

Overarching term that covers many drugs including those that increase activity of the central nervous system and the body, drugs that are pleasurable and invigorating, or drugs that have sympathomimetic effects.

Ritalin: 20 mg sustained-release (SR) tablets
A chart comparing the chemical structures of different amphetamine derivatives
Roasted coffee beans, a common source of caffeine.
Tablets containing MDMA
Lines of illicit cocaine, used as a recreational stimulant
Catha edulis

The most frequently prescribed stimulants as of 2013 were lisdexamfetamine (Vyvanse), methylphenidate (Ritalin), and amphetamine (Adderall).

People with ADHD may struggle more than others to focus on tasks such as schoolwork, but can maintain an unusually intense level of attention for tasks they find rewarding or interesting

Attention deficit hyperactivity disorder

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Neurodevelopmental disorder characterized by excessive amounts of inattention, hyperactivity, and impulsivity that are pervasive, impairing in multiple contexts, and otherwise age-inappropriate.

Neurodevelopmental disorder characterized by excessive amounts of inattention, hyperactivity, and impulsivity that are pervasive, impairing in multiple contexts, and otherwise age-inappropriate.

People with ADHD may struggle more than others to focus on tasks such as schoolwork, but can maintain an unusually intense level of attention for tasks they find rewarding or interesting
The left prefrontal cortex, shown here in blue, is often affected in ADHD.
Percent of people 4–17 ever diagnosed in the US as of 2011
Timeline of ADHD diagnostic criteria, prevalence, and treatment

Methylphenidate and amphetamine or its derivatives are first-line treatments for ADHD as they are considered the most effective pharmaceutical treatments.

The concentration of orexin-A neuropeptides in the cerebrospinal fluid of narcoleptic individuals is usually very low

Narcolepsy

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Long-term neurological disorder that involves a decreased ability to regulate sleep–wake cycles.

Long-term neurological disorder that involves a decreased ability to regulate sleep–wake cycles.

The concentration of orexin-A neuropeptides in the cerebrospinal fluid of narcoleptic individuals is usually very low

Medications used include modafinil, sodium oxybate and methylphenidate.

Skeletal formula of dopamine

Dopamine

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Neuromodulatory molecule that plays several important roles in cells.

Neuromodulatory molecule that plays several important roles in cells.

Skeletal formula of dopamine
Dopamine processing in a synapse. After release dopamine can either be taken up again by the presynaptic terminal, or broken down by enzymes.
TH: tyrosine hydroxylase
DOPA: L-DOPA
DAT: dopamine transporter
DDC: DOPA decarboxylase
VMAT: vesicular monoamine transporter 2
MAO: Monoamine oxidase
COMT: Catechol-O-methyl transferase
HVA: Homovanillic acid
Major dopamine pathways. As part of the reward pathway, dopamine is manufactured in nerve cell bodies located within the ventral tegmental area (VTA) and is released in the nucleus accumbens and the prefrontal cortex. The motor functions of dopamine are linked to a separate pathway, with cell bodies in the substantia nigra that manufacture and release dopamine into the dorsal striatum.
Main circuits of the basal ganglia. The dopaminergic pathway from the substantia nigra pars compacta to the striatum is shown in light blue.
Illustration of dopaminergic reward structures
Dopamine HCl preparation, single dose vial for intravenous administration
Cocaine increases dopamine levels by blocking dopamine transporters (DAT), which transport dopamine back into a synaptic terminal after it has been emitted.
Methamphetamine hydrochloride also known as crystal meth
Dopamine can be found in the peel and fruit pulp of bananas.

Cocaine, substituted amphetamines (including methamphetamine), Adderall, methylphenidate (marketed as Ritalin or Concerta), and other psychostimulants exert their effects primarily or partly by increasing dopamine levels in the brain by a variety of mechanisms.

Methamphetamine

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Potent central nervous system (CNS) stimulant that is mainly used as a recreational drug and less commonly as a second-line treatment for attention deficit hyperactivity disorder and obesity.

Potent central nervous system (CNS) stimulant that is mainly used as a recreational drug and less commonly as a second-line treatment for attention deficit hyperactivity disorder and obesity.

Desoxyn (Methamphetamine Hydrochloride) 100 tablets.
A 2010 study ranking various illegal and legal drugs based on statements by drug-harm experts. Methamphetamine was found to be the fourth most damaging to society.
A suspected case of meth mouth
This diagram depicts the neuroimmune mechanisms that mediate methamphetamine-induced neurodegeneration in the human brain. The NF-κB-mediated neuroimmune response to methamphetamine use which results in the increased permeability of the blood–brain barrier arises through its binding at and activation of sigma receptors, the increased production of reactive oxygen species (ROS), reactive nitrogen species (RNS), and damage-associated molecular pattern molecules (DAMPs), the dysregulation of glutamate transporters (specifically, EAAT1 and EAAT2) and glucose metabolism, and excessive Ca2+ ion influx in glial cells and dopamine neurons.
This illustration depicts the normal operation of the dopaminergic terminal to the left, and the dopaminergic terminal in the presence of methamphetamine to the right. Methamphetamine reverses the action of the dopamine transporter (DAT) by activating TAAR1 (not shown). TAAR1 activation also causes some of the dopamine transporters to move into the presynaptic neuron and cease transport (not shown). At VMAT2 (labeled VMAT), methamphetamine causes dopamine efflux (release).
Shards of pure methamphetamine hydrochloride, also known as crystal meth
Pervitin, a methamphetamine brand used by German soldiers during World War II, was dispensed in these tablet containers.
U.S. drug overdose related fatalities in 2017 were 70,200, including 10,333 of those related to psychostimulants (including methamphetamine).

It has been implicated in addictions to alcohol, cannabinoids, cocaine, methylphenidate, nicotine, opioids, phencyclidine, propofol, and substituted amphetamines, among others.

Chemical structure of morphine, the prototypical opioid.

Opioid

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Opioids are substances that act on opioid receptors to produce morphine-like effects.

Opioids are substances that act on opioid receptors to produce morphine-like effects.

Chemical structure of morphine, the prototypical opioid.
US. Top line represents the number of benzodiazepine deaths that also involved opioids. Bottom line represents benzodiazepine deaths that did not involve opioids.
Locants of the morphine molecule
INTA: selective agonist of KOR-DOR and KOR-MOR heteromers. Does not recruit β-arrestin II. Antinociceptive devoid of aversion, tolerance, and dependence in mice.
A sample of raw opium
US yearly deaths from all opioid drugs. Included in this number are opioid analgesics, along with heroin and illicit .<ref name=NIDA-deaths/>
US yearly deaths involving other, predominately Fentanyl.<ref name=NIDA-deaths/>
US yearly deaths involving prescription opioids. is a category dominated by illegally acquired fentanyl, and has been excluded.<ref name=NIDA-deaths>Overdose Death Rates. By National Institute on Drug Abuse (NIDA).</ref>
US yearly overdose deaths involving heroin.<ref name=NIDA-deaths/>

Stimulants (e.g. caffeine, modafinil, amphetamine, methylphenidate)

Modafinil is a common nootropic

Nootropic

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Nootropics (, or ) (colloquial: smart drugs and cognitive enhancers) are drugs, supplements, and other substances that are claimed to improve cognitive function, particularly executive functions, attention, memory, creativity, or motivation, in healthy individuals.

Nootropics (, or ) (colloquial: smart drugs and cognitive enhancers) are drugs, supplements, and other substances that are claimed to improve cognitive function, particularly executive functions, attention, memory, creativity, or motivation, in healthy individuals.

Modafinil is a common nootropic
Hebbian version of the Yerkes–Dodson law

Stimulants such as dimethylamylamine and methylphenidate are used on college campuses and by younger groups.

Novartis

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Swiss-American multinational pharmaceutical corporation based in Basel, Switzerland and

Swiss-American multinational pharmaceutical corporation based in Basel, Switzerland and

The Sandoz brand exists today as a subsidiary of Novartis.
Suffern, New York: one of the Novartis pharmaceutical production facilities in the United States
Novartis India headquarters in HITEC City, Hyderabad
Novartis in Cambridge, Massachusetts in November 2019.

Novartis manufactures the drugs clozapine (Clozaril), diclofenac (Voltaren; sold to GlaxoSmithKline in 2015 deal), carbamazepine (Tegretol), valsartan (Diovan), imatinib mesylate (Gleevec/Glivec), cyclosporine (Neoral/Sandimmune), letrozole (Femara), methylphenidate (Ritalin; production ceased 2020), terbinafine (Lamisil), deferasirox (Exjade), and others.

1 : 1 mixture (racemate)

Bupropion

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Atypical antidepressant primarily used to treat major depressive disorder and to support smoking cessation.

Atypical antidepressant primarily used to treat major depressive disorder and to support smoking cessation.

1 : 1 mixture (racemate)
Wellbutrin XL
Principal pathways of bupropion metabolism.
Comparison of steady-state plasma bupropion levels with bupropion IR 100 mg t.i.d. (3x/day), bupropion SR 150 mg b.i.d. (2x/day), and bupropion XL 300 mg q.d. (1x/day).

This is in contrast to stimulants, such as amphetamine and methylphenidate, which have an immediate onset of effect in the condition.